Abstract
A series of 1-(substituted biaryloxy)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl) propan-2-ol were synthesized and their antifungal activities were evaluated against eight human pathogenic fungi in vitro. Seventeen compounds showed activity 4- to 64-fold higher than voriconazole against Candida albicans. SAR clearly suggested that introduction of a biaryloxy side chain greatly enhanced the antifungal activity of triazole analogs against Candida species.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antifungal Agents / chemical synthesis*
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacology*
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Candida albicans / drug effects
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Fluconazole / pharmacology
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Humans
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Microbial Sensitivity Tests
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Molecular Structure
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Pyrimidines / pharmacology
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Structure-Activity Relationship
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Triazoles / chemical synthesis*
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Triazoles / chemistry
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Triazoles / pharmacology*
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Voriconazole
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Yeasts / drug effects
Substances
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Antifungal Agents
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Pyrimidines
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Triazoles
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Fluconazole
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Voriconazole